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Assay Detail

CHEMBL3630759

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Antagonist activity at human TRPV1 heterologously expressed in CHO cells assessed as inhibition of capsaicin-induced activation by FLIPR assay
ChEMBL ↗
72
Total Activities
72
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Transient receptor potential cation channel subfamily V member 1 (CHEMBL4794) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure activity relationships of benzyl C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists.
Ann J, Jung A, Kim MY, Kim HM, Ryu H, Kim S, Kang DW, Hong S, Cui M, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, Lee J.
Bioorg Med Chem (2015) 23 : 6844 -6854
PubMed 26474664 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 72 8.92 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2177440 — — 1 9.70
CHEMBL2178063 — — 1 9.70
CHEMBL3314389 — — 1 9.70
CHEMBL3629486 — — 1 9.52
CHEMBL3627950 — — 1 9.52
CHEMBL2177428 — — 1 9.52
CHEMBL3627723 — — 1 9.52
CHEMBL3629498 — — 1 9.40
CHEMBL3629227 — — 1 9.40
CHEMBL3629494 — — 1 9.40
CHEMBL3629497 — — 1 9.40
CHEMBL2177405 — — 1 9.40
CHEMBL2442912 — — 1 9.40
CHEMBL3627951 — — 1 9.30
CHEMBL3627953 — — 1 9.30
CHEMBL3627940 — — 1 9.30
CHEMBL3627944 — — 1 9.30
CHEMBL3629228 — — 1 9.22
CHEMBL3317476 — — 1 9.22
CHEMBL3627941 — — 1 9.22
CHEMBL3629233 — — 1 9.22
CHEMBL3629492 — — 1 9.15
CHEMBL3627937 — — 1 9.15
CHEMBL3627942 — — 1 9.15
CHEMBL3629501 — — 1 9.15
CHEMBL3627938 — — 1 9.10
CHEMBL3627939 — — 1 9.10
CHEMBL2385409 — — 1 9.10
CHEMBL3629229 — — 1 9.10
CHEMBL2442911 — — 1 9.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2177440 — Ki = 0.2 nM 9.70
CHEMBL2178063 — Ki = 0.2 nM 9.70
CHEMBL3314389 — Ki = 0.2 nM 9.70
CHEMBL3629486 — Ki = 0.3 nM 9.52
CHEMBL3627950 — Ki = 0.3 nM 9.52
CHEMBL2177428 — Ki = 0.3 nM 9.52
CHEMBL3627723 — Ki = 0.3 nM 9.52
CHEMBL3629498 — Ki = 0.4 nM 9.40
CHEMBL3629227 — Ki = 0.4 nM 9.40
CHEMBL3629494 — Ki = 0.4 nM 9.40
CHEMBL3629497 — Ki = 0.4 nM 9.40
CHEMBL2177405 — Ki = 0.4 nM 9.40
CHEMBL2442912 — Ki = 0.4 nM 9.40
CHEMBL3627944 — Ki = 0.5 nM 9.30
CHEMBL3627953 — Ki = 0.5 nM 9.30
CHEMBL3627951 — Ki = 0.5 nM 9.30
CHEMBL3627940 — Ki = 0.5 nM 9.30
CHEMBL3629228 — Ki = 0.6 nM 9.22
CHEMBL3317476 — Ki = 0.6 nM 9.22
CHEMBL3627941 — Ki = 0.6 nM 9.22
CHEMBL3629233 — Ki = 0.6 nM 9.22
CHEMBL3629492 — Ki = 0.7 nM 9.15
CHEMBL3627937 — Ki = 0.7 nM 9.15
CHEMBL3627942 — Ki = 0.7 nM 9.15
CHEMBL3629501 — Ki = 0.7 nM 9.15
CHEMBL3627938 — Ki = 0.8 nM 9.10
CHEMBL3629229 — Ki = 0.8 nM 9.10
CHEMBL3627939 — Ki = 0.8 nM 9.10
CHEMBL2385409 — Ki = 0.8 nM 9.10
CHEMBL2442911 — Ki = 0.9 nM 9.05
CHEMBL3629491 — Ki = 0.9 nM 9.05
CHEMBL2385416 — Ki = 0.9 nM 9.05
CHEMBL3627943 — Ki = 0.9 nM 9.05
CHEMBL3629495 — Ki = 0.9 nM 9.05
CHEMBL3629221 — Ki = 0.9 nM 9.05
CHEMBL3313936 — Ki = 1.0 nM 9.00
CHEMBL3629232 — Ki = 1.0 nM 9.00
CHEMBL3627936 — Ki = 1.0 nM 9.00
CHEMBL3629230 — Ki = 1.1 nM 8.96
CHEMBL3627954 — Ki = 1.1 nM 8.96
CHEMBL2442910 — Ki = 1.2 nM 8.92
CHEMBL3629361 — Ki = 1.2 nM 8.92
CHEMBL3629493 — Ki = 1.3 nM 8.89
CHEMBL3629496 — Ki = 1.4 nM 8.85
CHEMBL3627948 — Ki = 1.4 nM 8.85
CHEMBL3629489 — Ki = 1.6 nM 8.80
CHEMBL3627933 — Ki = 1.6 nM 8.80
CHEMBL3629488 — Ki = 1.7 nM 8.77
CHEMBL3627931 — Ki = 1.8 nM 8.74
CHEMBL3627947 — Ki = 1.8 nM 8.74